[CAS NO. 2376255-48-8]  Ac-FLTD-CMK

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PRODUCTS SPECIFICATIONS [2376255-48-8]

Catalog
HY-111675
Brand
MCE
CAS
2376255-48-8

DESCRIPTION [2376255-48-8]

Overview

MDL-
Molecular Weight569.05
Molecular FormulaC26H37ClN4O8
SMILESClCC([C@H](CC(O)=O)NC([C@H]([C@H](O)C)NC([C@H](CC(C)C)NC([C@@H](NC(C)=O)CC1=CC=CC=C1)=O)=O)=O)=O

For research use only. We do not sell to patients.


Summary

Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 ( IC 50 of 46.7 nM), caspases-4 ( IC 50 of 1.49 μM), caspases-5 ( IC 50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3 [1] .


IC50 & Target

Caspase-1

46.7 nM (IC 50 )

Caspase-4

1.49 μM (IC 50 )

Caspase-5

329 nM (IC 50 )

Caspase-11


In Vitro

Ac-FLTD-CMK, inhibits GSDMD cleavage by caspases-1, -4, -5, and -11 in vitro, suppresses pyroptosis downstream of both canonical and noncanonical inflammasomes, as well as reduces IL-1β release following activation of the NLRP3 inflammasome in macrophages. By contrast, Ac-FLTD-CMK does not target caspase-3 or apoptotic cell death. Crystal structure of caspase-1 in complex with Ac-FLTD-CMK reveals extensive enzyme-inhibitor interactions involving both hydrogen bonds and hydrophobic contacts [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 175.73 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7573 mL 8.7866 mL 17.5731 mL
5 mM 0.3515 mL 1.7573 mL 3.5146 mL
10 mM 0.1757 mL 0.8787 mL 1.7573 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

* All of the co-solvents are available by MCE.